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  2. Cetirizine - Wikipedia

    en.wikipedia.org/wiki/Cetirizine

    The K i values for the H 1 receptor are approximately 6 nM for cetirizine, 3 nM for levocetirizine, and 100 nM for dextrocetirizine, indicating that the levorotatory enantiomer is the main active form. [3] Cetirizine has 600-fold or greater selectivity for the H 1 receptor over a wide variety of other sites, including muscarinic acetylcholine ...

  3. Histamine receptor - Wikipedia

    en.wikipedia.org/wiki/Histamine_receptor

    H1 receptors are linked to allergic responses, H2 to gastric acid regulation, H3 to neurotransmitter release modulation, and H4 to immune system function. There are four known histamine receptors: H 1 receptor H1 Receptors: These receptors are primarily located on smooth muscle cells , endothelial cells, and neurons.

  4. H1 antagonist - Wikipedia

    en.wikipedia.org/wiki/H1_antagonist

    H 1 antagonists, also called H 1 blockers, are a class of medications that block the action of histamine at the H 1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines ; other agents may have antihistaminergic action but are ...

  5. Antihistamine - Wikipedia

    en.wikipedia.org/wiki/Antihistamine

    The first H 1 receptor antagonists were discovered in the 1930s and were marketed in the 1940s. [22] ... and cetirizine, that target histamine receptor H1 ...

  6. Histamine H2 receptor - Wikipedia

    en.wikipedia.org/wiki/Histamine_H2_receptor

    Its various actions are mediated by histamine receptors H 1, H 2, H 3 and H 4. The histamine receptor H 2 belongs to the rhodopsin-like family of G protein-coupled receptors. It is an integral membrane protein and stimulates gastric acid secretion.

  7. Histamine H1 receptor - Wikipedia

    en.wikipedia.org/wiki/Histamine_H1_receptor

    The H 1 receptor is a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors. This receptor is activated by the biogenic amine histamine . It is expressed in smooth muscles , on vascular endothelial cells , in the heart, and in the central nervous system .

  8. Levocetirizine - Wikipedia

    en.wikipedia.org/wiki/Levocetirizine

    It is classified as a second-generation antihistamine and works by blocking histamine H 1-receptors. [6] [3] Levocetirizine was approved for medical use in the United States in 2007, [3] and is available as a generic medication. [4] In 2022, it was the 152nd most commonly prescribed medication in the United States, with more than 3 million ...

  9. H2 receptor antagonist - Wikipedia

    en.wikipedia.org/wiki/H2_receptor_antagonist

    Like the H 1 antagonists, some H 2 antagonists function as inverse agonists rather than receptor antagonists, due to the constitutive activity of these receptors. [ 3 ] The prototypical H 2 antagonist, called cimetidine , was developed by Sir James Black [ 4 ] at Smith, Kline & French – now GlaxoSmithKline – in the mid-to-late 1960s.

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